Status:

COMPLETED

To Compare Blood and Urine Concentrations of Mirabegron (YM178) in Healthy Poor or Extensive Metabolizers for CYP2D6 and to Assess the Effect of Mirabegron on the Metabolism of Metoprolol

Lead Sponsor:

Astellas Pharma Inc

Conditions:

Pharmacokinetics of Mirabegron

Healthy Subjects

Eligibility:

MALE

18-55 years

Phase:

PHASE1

Brief Summary

The study aims to compare blood and urine concentrations of mirabegron (YM178) in healthy poor or extensive metabolizers for CYP2D6 and to evaluate if blood levels of metoprolol change whilst being do...

Detailed Description

The study is an open label, single center study. All subjects are genotyped for CYP2D6 before the study. Genotype expression is confirmed by dextromethorphan phenotyping. Part I: The pharmacokinetic ...

Eligibility Criteria

Inclusion

  • For Part I:
  • Subject genotyped and phenotyped for CYP2D6
  • Body weight between 60 and 100 kg and Body Mass Index less than or equal to 30 kg/m2
  • For Part II:
  • Subject genotyped and phenotyped as extensive metaboliser for CYP2D6
  • Body weight between 60 and 100 kg and Body Mass Index less than or equal to 30 kg/m2

Exclusion

  • Known or suspected hypersensitivity to β-adrenergic receptor agonists or constituents of the formulations used
  • Any clinically significant history of asthma, eczema, any other allergic condition or previous severe hypersensitivity to any drug
  • Any clinically significant history of upper gastrointestinal symptoms (such as nausea, vomiting, abdominal discomfort or upset, or heartburn) in the 4 weeks prior to admission to the Research Unit
  • Any clinically significant history of any other disease or disorder - gastrointestinal, cardiovascular, respiratory, renal, hepatic, neurological, dermatological, psychiatric or metabolic
  • Any clinically significant abnormality following the investigator's review of the pre-study physical examination, ECG and clinical laboratory tests
  • QTc intervals of \>430 msec
  • Abnormal pulse rate measurement (\<40 or \>90 bpm) taken by manual counting at the pre-study visit after subject has been resting in supine position for 5 min
  • Abnormal blood pressure measurements taken at the pre-study visit after subject has been resting in supine position for 5 min as follows: systolic blood pressure \<95 or \>160 mmHg; diastolic blood pressure \<40 or \>95 mmHg
  • Positive orthostatic test at screening i.e. any symptoms of dizziness, light-headedness etc. and/or a fall of ≥ 20 mmHg in systolic blood pressure after 2 min standing (preceded by 5 min. supine rest) and/or an increase in pulse rate of ≥ 20 bpm
  • Regular use of any prescribed or OTC drugs except paracetamol up to 3 g/day, in the 4 weeks prior to admission to the Research Unit OR any use of such drugs in the 2 weeks prior to admission to the Research Unit

Key Trial Info

Start Date :

September 1 2002

Trial Type :

INTERVENTIONAL

Allocation :

ACTUAL

End Date :

November 1 2002

Estimated Enrollment :

28 Patients enrolled

Trial Details

Trial ID

NCT01478490

Start Date

September 1 2002

End Date

November 1 2002

Last Update

April 10 2014

Active Locations (1)

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1

PRA International (former Pharma Bio-Research)

Zuidlaren, Netherlands, 9471 GP